Motilides, Macrolides with Gastrointestinal Motor Stimulating Activity. : II. Quaternary N-Substituted Derivatives of 8,9-Anhydroerythromycin A 6,9-Hemiacetal and 9,9-Dihydroerythromycin A 6,9-Epoxide
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概要
- 論文の詳細を見る
A series of quaternary ammonium derivatives of 8,9-anhydroerythromycin A 6,9-hemiacetal (1) and 9,9-dihydroerythromycin A 6,9-epoxide (2) has been prepared and tested for antimicrobial activity and gastrointestinal motor stimulating (GMS) activity in the dog (in vivo). The GMS activity is enhanced markedly when small alkyl halides and unsaturated alkyl halides such as allyl bromide and propargyl bromide are added to the dimethylamino group of 1. Among them, N-propargyl-8,9-anhydroerythromycin A 6,9-hemiacetal bromide (3) exhibits GMS activity 2890 times stronger than that of erythromycin A and is completely devoid of antimicrobial activity. The potency of 3 is comparable to that of synthetic motilin both in vitro and in vivo.
- 公益社団法人日本薬学会の論文
- 1989-10-25
著者
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大村 智
The Kitasato Institute
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豊田 元
The Kitasato Institute And School Of Pharmaceutical Sciences Kitasato University
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圓井 省吾
Pharmaceutical Research Laboratories III, Takeda Chemical Industries, Ltd.,
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砂塚 敏明
The Kitasato Institute and School of Pharmaceutical Science of Kitasato University
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続木 一夫
The Kitasato Institute and School of Pharmaceutical Science of Kitasato University
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圓井 省吾
The Kitasato Institute and School of Pharmaceutical Science of Kitasato University
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稲富 信博
College of Medical Technology of Gunma University
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伊藤 漸
College of Medical Technology of Gunma University
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圓井 省吾
Pharmaceutical Research Laboratories Iii Takeda Chemical Industries Ltd.
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続木 一夫
The Kitasato Institute And School Of Pharmaceutical Sciences Kitasato University
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砂塚 敏明
北里大 北里生命科研
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